Home Protein Tyrosine Kinase c-Met inhibitor AMG 337

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AMG 337 c-Met inhibitor

Cat.No.S8167

AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the Met (c-Met) receptor with an IC50 of 1 nM.
AMG 337 c-Met inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 463.46

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Quality Control

Batch: S816701 DMSO]95 mg/mL]false]Ethanol]95 mg/mL]false]Water]Insoluble]false Purity: 99.73%
99.73

Solubility

In vitro
Batch:

DMSO : 95 mg/mL (204.97 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 95 mg/mL

Water : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 463.46 Formula

C23H22FN7O3

 Storage (From the date of receipt)
CAS No. 1173699-31-4 Download SDF Storage of Stock Solutions

Synonyms N/A SMILES CC(C1=NN=C2N1C=C(C=C2F)C3=CN(N=C3)C)N4C=CC5=C(C4=O)C=C(C=N5)OCCOC

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Mechanism of Action

Targets/IC50/Ki
MET receptor
(Cell-free assay)
1 nM
MET(H1094R)
(Cell-free assay)
1 nM
MET(M1250T)
(Cell-free assay)
4.7 nM
MET(V1092I)
(Cell-free assay)
21.5 nM
In vitro
AMG 337 potently inhibits the enzymatic activity of WT MET and a subset of MET mutants found in papillary renal cell carcinoma. The inability of this compound to inhibit the Y1230 and D1228 mutants is likely the result of a disruption of the inactive confirmation of the activation loop in the MET kinase domain. It also inhibits cell based HGF-induced MET phosphorylation in PC3 cells with IC50 of 5nM. This compound inhibits proliferation in MET-dependent cancer cell lines. It inhibits signaling through the PI3K and MAPK pathways in MET-amplified gastric cancer cell lines resulting in profound effects on cell proliferation and survival.
In vivo
AMG 337 exhibits impressive potency with >90% inhibition of Gab-1 phosphorylation at a dose of 0.75 mg/kg (32 nmol/L free-drug concentration). This compound is well tolerated at continuously administered doses that corresponded with complete MET inhibition for 24 hours, suggesting that it has the preclinical attributes required to test the role of MET in human cancer.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-24)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03132155 TERMINATED
Clear Cell Sarcoma
NantPharma, LLC
 2018-08-29 PHASE2
NCT03147976 WITHDRAWN
Solid Tumor
NantPharma, LLC
 2018-05-02 PHASE2
NCT02016534 TERMINATED
Stomach Neoplasms
Amgen
 2014-02 PHASE2
NCT02096666 COMPLETED
Stomach Neoplasms
Amgen
 2014-04-15 PHASE1; PHASE2
NCT01253707 COMPLETED
Advanced Malignancy; Advanced Solid Tumors; Cancer; Oncology; Oncology Patients; Tumors
Amgen
 2010-12-08 PHASE1
NCT02344810 WITHDRAWN
Adenocarcinoma of the Esophagus; Adenocarcinoma of the Gastroesophageal Junction; Diffuse Adenocarcinoma of the Stomach; Gastrointestinal Cancer; Intestinal Adenocarcinoma of the Stomach; Mixed Adenocarcinoma of the Stomach; Stage IIIA Esophageal Cancer; Stage IIIA Gastric Cancer; Stage IIIB Esophageal Cancer; Stage IIIB Gastric Cancer; Stage IIIC Esophageal Cancer; Stage IIIC Gastric Cancer; Stage IV Esophageal Cancer; Stage IV Gastric Cancer
Eastern Cooperative Oncology Group
 2015-03-06 PHASE1; PHASE2

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